Search Result
Results for "
Oligomerization
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-145580
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- HY-129122
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VBIT-4
Maximum Cited Publications
8 Publications Verification
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VDAC
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Cardiovascular Disease
Neurological Disease
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VBIT-4 is an inhibitor of voltage-dependent anion channel 1 (VDAC1) oligomerization with a binding affinity (Kd) of 17 μM. VBIT-4, as an apoptosis inhibitor, can be used for therapeutic purposes in apoptosis-associated disorders, such as neurodegenerative and cardiovascular diseases .
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- HY-161296
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Bacterial
HIV
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Infection
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TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe .
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- HY-149237
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- HY-156179
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Amyloid-β
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Neurological Disease
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DDC 2′,3′-O-disulfate (compound 4) prevents the fibrillization and oligomerization of Aβ42. DDC 2′,3′-O-disulfate has the potential for Alzheimer's disease (AD) research .
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- HY-156180
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Drug Metabolite
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Neurological Disease
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DDC 3′-O-β-D glucuronide (compound 5) is a drug metabolite that can prevent the fibrillization and oligomerization of Aβ42. DDC 3′-O-β-D glucuronide has potential for the research of Alzheimer's disease .
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- HY-101112
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HuR
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Inflammation/Immunology
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Okicenone is a Hu protein R (HuR) inhibitor. Okicenone inhibits HuR oligomerization, interferes with HuR RNA binding, HuR trafficking, cytokine expression and T-cell activation .
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- HY-17406S
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Ro 40-7592 d7
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Isotope-Labeled Compounds
COMT
Amyloid-β
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Neurological Disease
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Tolcapone-d7 is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells[1][2].
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- HY-156374
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NOD-like Receptor (NLR)
Pyroptosis
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Inflammation/Immunology
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D359-0396 is an orally active NLRP3 inflammasome inhibitor. D359-0396 inhibits pyroptosis and IL-1β release in macrophages. D359-0396 also inhibits the oligomerization of NLRP3, ASC and the cleavage of GSDMD. D359-0396 alleviates EAE, and also improves survival after septic shock in mice .
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- HY-149604
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NLRP3-IN-21 (compound L38) is a NLRP3 inflammasome inhibitor with inflammatory properties. NLRP3-IN-21 inhibits NLRP3 inflammasome activation and pyroptosis by suppressing gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly .
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- HY-120079
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MSN-125
2 Publications Verification
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Bcl-2 Family
Apoptosis
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Cancer
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MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity .
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- HY-161242
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Bcl-2 Family
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Cancer
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CBI1 is a covalent BAX inhibitor. CBI1 selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 blocks t-2-hex lipidation and oligomerization of BAX. CBI1 inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
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- HY-136735
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IRE1
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Neurological Disease
Cancer
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IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM) .
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- HY-U00460
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IRE1
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Cancer
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3,6-DMAD hydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer .
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- HY-U00460B
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IRE1
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Cancer
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3,6-DMAD dihydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer .
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- HY-144226
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NOD-like Receptor (NLR)
AIM2
Pyroptosis
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Inflammation/Immunology
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NLRP3/AIM2-IN-3 (compound 59) is a potent inhibitor with differential species specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. NLRP3/AIM2-IN-3 shows inhibitory efficacy against pyroptosis in THP-1 macrophages stimulated with LPS/nigericin, with an IC50 of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disturbs the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization .
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- HY-108937
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- HY-145580A
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(S)-UCB0599; (S)-NPT200-11
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α-synuclein
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Neurological Disease
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(S)-Minzasolmin is an isomer of minzasolmin (HY-145580), an inhibitor of α-synuclein oligomerization .
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- HY-118948
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Bcl-2 Family
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Neurological Disease
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MSN-50 is a Bax and Bak oligomerization inhibitor. MSN-50 efficiently inhibits liposome permeabilization, prevents genotoxic cell death and promotes neuroprotection .
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- HY-161743
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AUTOTACs
Autophagy
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Cancer
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PBA-1105 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 increases the autophagic flux of Ub-conjugated aggregates .
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- HY-161744
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AUTOTACs
Autophagy
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Cancer
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PBA-1106 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1106 increases the autophagic flux of Ub-conjugated aggregates .
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- HY-161742
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- HY-18633
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Apoptosis
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Cancer
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MDK83190 is a potent apoptosis activator, induces Apaf-1 oligomerization, increases procaspase-9 processing and subsequent caspase-3 activation in a cyto c-dependent Manner .
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- HY-100691
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- HY-119519
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Others
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Neurological Disease
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OB-2 is a STOML3 oligomerization blocker. OB-2 reverses pathological mechanical hypersensitivity. OB-2 can be used for research of painful diabetic neuropathy in mice .
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- HY-18937
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RIP kinase
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Cancer
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WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation .
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- HY-103349
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PETCM
1 Publications Verification
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Caspase
Apoptosis
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Cancer
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PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells .
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- HY-122671
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Others
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Neurological Disease
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OB-1 is a stomatin-like protein-3 (STOML3) oligomerization blocker. OB-1 is an effective inhibitor of the self-association of Stomatin, STOML1 and STOML2, but not podocin .
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- HY-149233
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- HY-158405
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SARS-CoV
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Infection
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PAV-104 inhibits SARS-CoV-2 replication, with the MOI of 0.01. PAV-104 can interact with SARS-CoV-2 nucleocapsid (N) and interfered with its oligomerization, blocking particle assembly .
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- HY-100112
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RIP kinase
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Others
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WEHI-345 analog is the analog of WEHI-345. WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation .
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- HY-163358
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- HY-150147
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RAD51
Apoptosis
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Cancer
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CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a Kd of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis .
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- HY-123572
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- HY-W688687
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Autophagy
p62
Atg8/LC3
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Others
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XIE62-1004-A is an inducer of p62-LC3 interaction. XIE62-1004-A can bind to the ZZ-domain of p62, inducing p62 oligomerization and activating p62-dependent autophagy .
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- HY-17406
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Ro 40-7592
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COMT
Amyloid-β
Apoptosis
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Neurological Disease
Cancer
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Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver . Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis . Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma .
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- HY-161745
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AUTOTACs
p62
Autophagy
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Cancer
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PBA-1105b is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105b increases the autophagic flux of Ub-conjugated aggregates. PBA-1105b is a drastically longer PEG-based linker than PBA-1105 .
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- HY-136555
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells .
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- HY-18509
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IRE1
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Cancer
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IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines .
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- HY-161740
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AUTOTACs
Estrogen Receptor/ERR
Autophagy
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Cancer
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PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization and degradation of estrogen receptor ERβ (DC50:~2 nM, HEK293T). PHTPP-1304 also induces the formation of p62 +ERβ + puncta that are affected by autophagic flux in a dose-dependent manner .
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- HY-168159
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Toll-like Receptor (TLR)
NOD-like Receptor (NLR)
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Inflammation/Immunology
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TLR7 agonist 27 (compound 24) is a potent TLR7 agonist with an EC50 of 238.1 nM. TLR7 agonist 27 shows weak agonistic activity against NOD2 (nucleotide-binding oligomerization domain 2) (EC50 of 6.2 μM). TLR7 agonist 27 is a potent immunostimulant, and can be used as a vaccine adjuvant and/or immunotherapeutic .
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- HY-17406S1
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Ro 40-7592-d4
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Isotope-Labeled Compounds
COMT
Amyloid-β
Apoptosis
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Neurological Disease
Cancer
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Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
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- HY-100432
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LOC14
2 Publications Verification
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PDI
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Neurological Disease
Inflammation/Immunology
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LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
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- HY-17406R
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Ro 40-7592 (Standard)
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COMT
Amyloid-β
Apoptosis
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Neurological Disease
Cancer
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Tolcapone (Standard) is the analytical standard of Tolcapone. This product is intended for research and analytical applications. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver . Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis . Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma .
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- HY-161242A
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Bcl-2 Family
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Cancer
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CBI1 formic is a covalent BAX inhibitor. CBI1 formic selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 formic blocks t-2-hex lipidation and oligomerization of BAX. CBI1 formic inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
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- HY-149393
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Mixed Lineage Kinase
RIP kinase
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Cancer
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RIPK3-IN-3 (compound 20) is a selective inhibitor of RIP kinase RIPK3 (IC50=10 nM). RIPK3 mediates the phosphorylation of Mixed Lineage Kinase (MLKL) and causes necroptosis, while RIPK3-IN-3 inhibits p-MLKL oligomerization and thereby inhibits necroptosis. RIPK3-IN-3 also downregulates CXCL5 secretion and inhibits AsPC-1 cell migration and invasion .
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- HY-157214
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STING
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Cancer
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NVS-STG2 is a molecular glue that targets STING and activates STING-mediated immune signaling. NVS-STG2 induces higher-order oligomerization of human STING by binding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models .
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- HY-156119
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Mixed Lineage Kinase
Necroptosis
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Metabolic Disease
Cancer
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MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor targeting Mixed Lineage Kinase domain-like (MLKL). MLKL-IN-6 inhibits cell necrosis. MLKL-IN-6 inhibits MLKL phosphorylation and oligomerization during cell necrosis, inhibits immune cell death, and reduces the expression of adhesion factors. MLKL-IN-6 has low cytotoxicity, and it inhibits hepatic stellate cell activation, reduces liver fibrosis marker levels, and has anti-fibrotic effects .
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- HY-161072
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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CSC-6 is a NLRP3 inhibitor. CSC-6 can significantly inhibit IL-1β secreted by PMATHP-1 cells with an IC50 value of 2.3 μM. CSC-6 specifically binds NLRP3 and inhibits NLRP3 activation by blocking ASC oligomerization during NLRP3 assembly. CSC-6 effectively reduces the symptoms of NLRP3 overactivation-mediated sepsis and gout in mouse models .
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- HY-146034
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NOD-like Receptor (NLR)
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Inflammation/Immunology
Cancer
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NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding
oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX) .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P5334A
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Peptides
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Neurological Disease
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AADvac 1 TFA is an active tau peptide vaccine for Alzheimer's disease research. AADvac 1 TFA is composed of a regulatory peptide 294KDNIKHVPGGGS 305 that drives tau oligomerization conjugated to Aplysia hemocyanin (KLH) and formulated with aluminum hydroxide .
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- HY-P5334
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Peptides
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Neurological Disease
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AADvac 1 is an active tau peptide vaccine for Alzheimer's disease research. AADvac 1 is composed of a regulatory peptide 294KDNIKHVPGGGS 305 that drives tau oligomerization conjugated to Aplysia hemocyanin (KLH) and formulated with aluminum hydroxide .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-17406S1
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Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
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- HY-17406S
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Tolcapone-d7 is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells[1][2].
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